Betahistine: Uses, Administration, Side Effects, Contraindications, Interactions and Frequently Asked Questions

It belongs to a group of medicines used to treat vertigo associated with Ménière’s disease.

The vertigo is a condition that causes patients to have a feeling of rotation or movement of themselves or their environment.

Ménière’s disease is an inner ear disorder that causes vertigo in addition to symptoms such as ringing in the ears, headache, and hearing loss.

It is similar to a natural substance called histamine . This medicine is not recommended in patients with pheochromocytoma.

Betahistine is used to reduce the number of vertigo episodes associated with Ménière’s disease. It is believed to work by lowering the pressure in the ear.

This pressure is thought to contribute to the feeling of dizziness, nausea, and ringing in the ears and hearing loss that people with Ménière’s disease experience.

Forms that this medicine has

16 mg

Each round, biconvex, scored, white or almost white tablet with bevelled edges, debossed with ‘N’ on one side and ‘267’ on the marked side, contains 16 mg betahistine.

Non-medicinal ingredients: mannitol, microcrystalline cellulose, and sodium stearyl fumarate.

24 mg

Each round, biconvex, scored, white or almost white tablet with bevelled edges, debossed with ‘N’ on one side and ’24’ on the marked side, contains 24 mg betahistine.

Non-medicinal ingredients: mannitol, microcrystalline cellulose, and sodium stearyl fumarate.

How to take betahistine?

The usual recommended dose of betahistine for adults is 24 mg to 48 mg given in 2 or 3 divided doses (i.e. 12 mg to 24 mg twice a day, or 8 mg to 16 mg three times a day). To prevent stomach upset, it is recommended to take this medication with food.

Before starting treatment, read the manufacturer’s printed information leaflet from inside the package. It will give you more information about betahistine and also provide you with a complete list of the side effects you might experience from taking it.

Take betahistine exactly as your doctor tells you. It is usual to take a 16 mg tablet three times a day at first. Once your symptoms are under control, your doctor may reduce your dose to one 8 mg tablet three times a day.

You will find the instructions for taking the tablets on the package label to remind you of what the doctor told you. Wherever possible, take betahistine tablets with something to eat, as a snack or directly after a meal.

Swallow the tablet with a drink of water. Try to take your doses at the same time of day each day, as this will help you remember to take the tablets regularly.

If you forget to take a dose, don’t worry, just remember to take the next dose when it is time. Do not take two doses together to make up for a forgotten dose.

Side effects

  • Sickness.
  • Headache.
  • Indigestion.
  • Swelling.
  • Acne.
  • Trouble sleeping
  • Fast heartbeat
  • Difficulty breathing.
  • Itch.
  • Stomach ache.

Frequently asked questions about betahistine

Start of action

Not enough information is available on the maximum levels of this drug in the body. The presence of food can delay the absorption of this medicine.

Duration of effect

The effect of this medicine has an average duration of 16 to 17 hours.

Is it safe with alcohol?

Interaction with alcohol is unknown. It is advisable to consult your doctor before consumption.

Can you form a habit?

Habit formation trends were reported.

Use in pregnancy?

This medication is not recommended for pregnant women unless absolutely necessary.

Use during lactation?

This medication is not recommended for women who are breastfeeding unless absolutely necessary.

Contraindications of betahistine

Pheochromocytoma

This drug is not recommended in patients with a condition called pheochromocytoma.

Allergy

This medicine is not recommended in patients with a known history of allergy to betahistine.

Missed dose

If you miss a dose of betahistine, take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose. Do not double your dose to make up for a forgotten dose.

Overdose

Seek emergency medical treatment or contact doctor in case of overdose.

General warnings

Gastrointestinal disorder:  This drug may increase the risk of stomach ulcers. Tell your doctor if you have a history of peptic ulcer disease or any gastrointestinal disease. Drink adequate amount of water to avoid stomach irritation.

Asthma:  This medicine can increase the risk of breathing problems. Tell your doctor if you have a history of asthma or any lung disease.

Impaired liver function:  Injury to the liver can cause this drug to build up in the body. Any history of liver disease should be reported to the doctor and necessary precautions taken to prevent further accumulation.

Pediatric Use: This medicine is not recommended for children under 18 years of age.

Get the most out of your treatment

If you are a driver, you must stop driving when Ménière’s disease is diagnosed. This is because you may have sudden attacks of a spinning sensation (vertigo) with little warning. Taking betahistine will not affect your ability to drive.

If you take betahistine every day, it is unlikely that it will stop all attacks, but it may reduce the number and / or severity of your attacks. Your doctor may recommend a betahistine trial for 6-12 months to see if it helps reduce your symptoms. If it does, it can be continued.

Some people with Ménière’s disease report that their symptoms improve with a low-salt diet, regular exercise, quitting smoking, and eliminating caffeine and alcohol. Although there is little evidence that diet and lifestyle can help, it may be worth a try.

If you buy any medications, ask a pharmacist if it is appropriate to take them with betahistine. Betahistine may not be as effective when taken together with a medicine that contains an antihistamine .

Pharmacology

Betahistine is a strong antagonist of the histamine H3 receptor and a weak agonist of the histamine H1 receptor.

Betahistine has two mechanisms of action. Primarily, it is a full agonist at H1 receptors located on blood vessels in the inner ear.

This results in local vasodilation and increased permeability, helping to reverse the underlying problem of endolymphatic hydrops.

More importantly, betahistine has a powerful antagonistic effect on H3 receptors, increasing the levels of the neurotransmitters histamine, acetylcholine, norepinephrine, serotonin, and GABA released from nerve endings.

The increased amounts of histamine released by histaminergic nerve endings can stimulate the receptors. This stimulation explains the potent vasodilatory effects of betahistine in the inner ear, which are well documented.

It is postulated that the increase of betahistine in the level of serotonin in the brainstem inhibits the activity of the vestibular nuclei.

Interactions

Betahistine may interact with the following medications and products:

Monoamine oxidase inhibitors: Betahistine blood levels may increase when taken with monoamine oxidase inhibitors such as moclobemide, phenelzine, and selegiline for the treatment of depression.

This interaction can cause serious effects. Inform the doctor and change the medicine or modify your dose.

Antihistamines: tell  your doctor if you are receiving anti-allergy medicines or cough preparations that contain antihistamines such as diphenhydramine, cetirizine, chlorpheniramine, as they are betahistine antagonists.

Beta-2 agonists: betahistine can decrease the effect of bronchodilators. Inform your doctor if you are receiving a Beta-2 agonist, as in this case, a dose alteration or substitution of a medicine may be necessary.

Precautions

Here are some precautions to keep in mind before taking betahistine:

The medicine can make the symptoms of breathing problems worse; therefore, talk to your doctor if you have asthma.

Liver disease can cause drugs to build up in the body, causing more side effects.

Betahistine can lead to an increase in symptoms associated with a stomach ulcer. You should have a detailed discussion with your doctor about the effect the medicine may have on you if you have a stomach ulcer and if you need any special monitoring.

It is advisable not to use this medicine if you are pregnant.

Medicines containing betahistine

Below is the list of drugs that contain betahistine as an ingredient:

  • Vertin 8 mg Tablet.
  • Vertiford 16 mg Tableta.
  • Zevert 8 mg Tableta.
  • Vertiford 8 mg Tableta.
  • Meneas 8 mg Tableta.
  • Betavert 16 mg Tableta.
  • Verbet 16 mg Tableta.
  • Vertilet 16 mg Tableta.
  • Stablanz Pv Tablet.
  • Vernil Plus Tablet.
  • Merislon 6 mg Tablets.
  • Avert 8 mg Tableta.
  • Verbet 8 mg Tableta.
  • Zevert 16 mg Tableta.
  • Betavert 24 mg Tableta.
  • Betavert 48 mg Tableta.
  • Vertipress 24 mg Tableta.
  • Divert 16 mg Tableta.
  • Vertin 48 mg Tablet.
  • Orgahist 16 mg Tablets.
  • Vertin 16 mg Tablet.

Availability

Betahistine is widely used and available in Europe, mainly in the UK. Betahistine is used by 94% of physicians in the UK.

The brand Serc (betahistine) was approved by the US FDA approximately 50 years ago in the early 1970s for approximately 5 years as a vestibular suppressant, for Ménière’s disease.

However, its approval was subsequently withdrawn due to lack of evidence of efficacy because the main effectiveness report contained deficiencies and misrepresentations. The withdrawal was confirmed by a United States court of appeals in 1968.

The Serc brand is not sold through common US pharmacy chains, but can be obtained through some US pharmacies, and some Walgreens, with a prescription. Some insurances can cover it too. Betahistine can also be easily obtained through foreign pharmacies.